发明名称 DERIVATIVES OF 8-OXO-5,8-DIHYDRO-6H-DIBENZO[A,G]QUINOLIZINE-13-PROPANOIC ACID, METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION
摘要 organic chemistry pharmacy. SUBSTANCE: invention relates to compounds of the general formula (I) where X means hydrogen or halogen atom, (C1-C3)-alkyl group, one or two (C1-C3)-alkoxy-groups or trifluoromethyl-group; Y is hydrogen or halogen atom, (C1-C3)-alkyl or (C1-C3)-alkoxy-group; R means hydroxy-group, methoxy-group or group of the general formula NR2R3 where R2 and R3 each means independently hydrogen atom, (C1-C4)-alkyl group, 2-methoxyethyl group, 3-methoxyethyl group, 3-aminopropyl group, group 2-(dimethylamino)ethyl, group 3-(dimethylamino)propyl or group 2-piperidine-2-yl-ethyl; or R2 and R3 in common with nitrogen atom with which they are bound form morpholine, pyrrolidine or piperazine ring that can has a substituent at position 4 as methyl group or group (1,1-dimethylethoxy)carbonyl, as free base or salt formed by acid addition. Compounds of the formula (I) show activity of binding ω-benzodiazepine receptors associated with GABAA-receptors and can be used in therapy as drugs for treatment of diseases associated with disorder of GABAA-ergic transfer of GABAA-receptors by subunits alpha1, alpha2, alpha3, alpha5. Invention proposes also method of synthesis of indicated compounds and pharmaceutical composition based on said. EFFECT: improved method of synthesis and preparing, valuable medicinal properties. 4 cl, 1 tbl, 3 dwg, 5 ex
申请公布号 RU2155764(C2) 申请公布日期 2000.09.10
申请号 RU19950122601 申请日期 1995.12.28
申请人 SINTELJABO 发明人 SEVREN MIREJ;FRUASSAN ZHAK;MARABU BENUA;DASHARI EHMMANJUEHLL'
分类号 C07D455/03;A61K31/435;A61K31/445;A61K31/47;A61K31/4745;A61K31/495;A61K31/496;A61K31/535;A61K31/5377;A61P5/02;A61P21/02;A61P25/00;A61P25/04;A61P25/18;A61P25/20;A61P25/24;A61P25/26;A61P25/30;C07D455/02;(IPC1-7):C07D455/03;A61K31/474;A61K31/537 主分类号 C07D455/03
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